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dc.contributor.authorNikiforov, Petaren
dc.contributor.authorBlaszczyk, Michalen
dc.contributor.authorSurade, Sen
dc.contributor.authorBoshoff, HIen
dc.contributor.authorSajid, Aen
dc.contributor.authorDelorme, Ven
dc.contributor.authorDeboosere, Nen
dc.contributor.authorBrodin, Pen
dc.contributor.authorBaulard, ARen
dc.contributor.authorBarry, CEen
dc.contributor.authorBlundell, Tomen
dc.contributor.authorAbell, Chrisen
dc.date.accessioned2017-06-23T14:32:11Z
dc.date.available2017-06-23T14:32:11Z
dc.date.issued2017-05-19en
dc.identifier.issn1554-8929
dc.identifier.urihttps://www.repository.cam.ac.uk/handle/1810/264980
dc.description.abstractSmall-molecule inhibitors of the mycobacterial transcriptional repressor EthR have previously been shown to act as boosters of the second-line antituberculosis drug ethionamide. Fragment-based drug discovery approaches have been used in the past to make highly potent EthR inhibitors with ethionamide boosting activity both $\textit{in vitro}$ and $\textit{ex vivo}$. Herein, we report the development of fragment-sized EthR ligands with nanomolar minimum effective concentration values for boosting the ethionamide activity in $\textit{Mycobacterium tuberculosis}$ whole-cell assays.
dc.description.sponsorshipWe would like to thank A. Coyne for help in the preparation of this manuscript. P.O.N. would like to thank the EPSRC for providing Ph.D. funding. We also thank the Bill and Melinda Gates Foundation and the EU FP7MM4TB Grant No. 260872, the ERC-STG INTRACELLTB Grant No. 260901, the Agence Nationale de la Recherche (ANR-10-EQPX-04-01), the Feder (12001407 (D-AL) Equipex Imaginex BioMed), the Intramural Research Program of the National Institutes of Health/NIAID, and the Région Nord Pas de Calais, France, for providing funding to support this work.
dc.languageengen
dc.language.isoenen
dc.publisherAmerican Chemical Society
dc.rightsAttribution 4.0 Internationalen
dc.rightsAttribution 4.0 Internationalen
dc.rightsAttribution 4.0 Internationalen
dc.rightsAttribution 4.0 Internationalen
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.titleFragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell $\textit{Mycobacterium tuberculosis}$ Assaysen
dc.typeArticle
prism.endingPage1396
prism.issueIdentifier5en
prism.publicationDate2017en
prism.publicationNameACS Chemical Biologyen
prism.startingPage1390
prism.volume12en
dc.identifier.doi10.17863/CAM.10841
dcterms.dateAccepted2017-03-17en
rioxxterms.versionofrecord10.1021/acschembio.7b00091en
rioxxterms.versionVoRen
rioxxterms.licenseref.urihttp://creativecommons.org/licenses/by/4.0/en
rioxxterms.licenseref.startdate2017-05-19en
dc.contributor.orcidBlundell, Tom [0000-0002-2708-8992]
dc.contributor.orcidAbell, Chris [0000-0001-9174-1987]
dc.identifier.eissn1554-8937
rioxxterms.typeJournal Article/Reviewen
pubs.funder-project-idEC FP7 CP (260872)
pubs.funder-project-idBill & Melinda Gates Foundation (via Foundation for the National Institutes of Health (FNIH)) (ABELL11HTB0)
pubs.funder-project-idEPSRC (EP/K039520/1)
cam.issuedOnline2017-03-17en
cam.orpheus.successThu Jan 30 12:53:50 GMT 2020 - The item has an open VoR version.*
rioxxterms.freetoread.startdate2100-01-01


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Attribution 4.0 International
Except where otherwise noted, this item's licence is described as Attribution 4.0 International